Reaktion #2371225

Reaktionsgleichung

4-Amino-6-{4-[1-(2-azetidin-1-yl-ethyl)-4-(4-fluoro-3-methoxy-phenyl)-1H-imidazol-2-yl]-piperidin-1-yl}-pyrimidine-5-carbonitrile

H2O2

NaOH

→

4-amino-6-(4-(1-(2-(azetidin-1-yl)ethyl)-4-(4-fluoro-3-methoxyphenyl)-1H-imidazol-2-yl)piperidin-1-yl)pyrimidine-5-carboxamide

Lösungsmittel

DMSO

Reaktionsbedingungen

Aufarbeitung

1. 1
   workup.STIRRING2.0MNaOH aq (1.05 ml; 2.10 mmol; 10.00 eq.), stirred at RT for 2 hr
2. 2
   Sonstigepurified the product by prep HPLC (basic), title compound 66 mg, 63%

Vorschrift

A reaction mixture of 4-Amino-6-{4-[1-(2-azetidin-1-yl-ethyl)-4-(4-fluoro-3-methoxy-phenyl)-1H-imidazol-2-yl]-piperidin-1-yl}-pyrimidine-5-carbonitrile (100.00 mg; 0.21 mmol; 1.00 eq.), DMSO 8 ml was stirred at RT added H2O2 (0.20 ml; 2.10 mmol; 10.00 eq.) and 2.0M NaOH.2.0MNaOH aq (1.05 ml; 2.10 mmol; 10.00 eq.), stirred at RT for 2 hr, got desired as major detected by lc-ms, purified the product by prep HPLC (basic), title compound 66 mg, 63%. LC-MS (M+1=495, obsd.=495).

Quelle